Intrarectal pharmacokinetics of two formulations of quinine in children with falciparum malaria

• Published in: European journal of clinical pharmacology Vol. 58; no. 10; pp. 649 - 652
• Main Authors: BARENNES, H, STERLINGOT, H, NAGOT, N, MEDA, H, KABORE, M, SANOU, M, NACRO, B, BOUREE, P, PUSSARD, E
• Format: Journal Article
• Language: English
• Published: Heidelberg Springer 01.02.2003; Berlin Springer Nature B.V
• Subjects: Acute Disease; Administration, Oral; Administration, Rectal; Africa; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antimalarials - administration & dosage; Antimalarials - blood; Antimalarials - pharmacokinetics; Antiparasitic agents; Area Under Curve; Biological and medical sciences; Biological Availability; Child; Child, Preschool; Humans; Infusions, Intravenous; Malaria; Malaria, Falciparum - blood; Malaria, Falciparum - drug therapy; Medical sciences; Pharmacology. Drug treatments; Quinine - administration & dosage; Quinine - blood; Quinine - pharmacokinetics; Time Factors; Africa; Antimalarial; Protozoal disease; Cinchona; Intravenous administration; Intrarectal administration; Alkaloid; Dicotyledones; Formulation; Angiospermae; Rubiaceae; Parasiticid; Child; Human; Malaria; Quinine hydrochloride salt; Childhood malaria; Parasitosis; Quinine; Rectal administration; Infection; Chemotherapy; Treatment; Antipyretic; Dosage form; Spermatophyta; Pharmacokinetics; Cinchona alkaloid mixture; Comparative study
• ISSN: 0031-6970; 1432-1041
• DOI: 10.1007/s00228-002-0546-2

To compare the intrarectal bioavailabilities of two parenteral formulations of quinine most available in French- (Cinchona alkaloid mixture) and English (hydrochloride salt) -speaking areas of Africa. The pharmacokinetics of quinine was investigated in four groups of 12 children with acute Plasmodium falciparum malaria receiving 8 mg/kg quinine base every 8 h either as hydrochloride salt or Cinchona alkaloid mixture by a slow 4-h intravenous infusion or intrarectal administration. Body temperature and parasitaemia were monitored, and blood quinine concentrations were measured by means of high-performance liquid chromatography. At 72 h, all the children were aparasitaemic and apyretic. Quinine C(max) values were higher after intravenous infusion of the hydrochloride salt and Cinchona alkaloid mixture (6.9+/-1.9 micro g/ml and 5.2+/-1.3 micro g/ml) than after intrarectal administration (3.5+/-1.4 micro g/ml and 3.1+/-1.6 micro g/ml), but t(max) values were similar (3.6+/-1.5, 4.2+/-1.0, 4.0+/-1.9, and 4.7+/-2.0 h, respectively). Intrarectal relative bioavailabilities of hydrochloride salt solution (57%) and Cinchona alkaloid mixture (62%) were similar. Whatever the parenteral formulation of quinine, the blood concentration-time profiles of quinine were similar after intrarectal administration. Intrarectal administration of hydrochloride salt solution is a possible mode of quinine delivery in remote rural areas of Africa.